ExpressPlus CYP Inhibition in Human Liver Microsomes Using LC-MS/MS

This assay is used to screen for reversible inhibition of individual cytochrome P450 (CYP) enzymes by a single concentration of a test compound

Catalog number EA426

Required from Customer

Deliverables

Substrate

Assay System

Assay Conditions

Assay QC

Notes

  1. The results from this assay are sent to the customer in the ExpressPlus report format, which may include graphical representations of data and comparison with historical data for reference compounds.
  2. Percent inhibition is calculated from the amount of metabolite formed in the presence of test compound relative to that formed in the absence of test compound, based on the peak area response ratio (PARR): % Inhibition = [(PARR without test compound - PARR with test compound) / (PARR without test compound)] x 100%.
Individual CYP Substrates and Positive Control Inhibitors 
CYP Isoform Probe Substrate Metabolite Positive Control Inhibitor
1A2 Phenacetin Acetaminophen α-Naphthoflavone
2A6 Coumarin 7-OH coumarin Tranylcypromine
2B6 Bupropion Bupropion Thio-TEPA
2C8 Amodiaquine Desethylamodiaquine Montelukast
2C9 Diclofenac 4’-OH diclofenac Sulfaphenazole
2C19 S-mephenytoin 4’-OH mephenytoin (+)-N-3-benzylnirvanol
2D6 Bufuralol 1’-OH bufuralol Quinidine
2E1 Chlorzoxazone 6-OH chlorzoxazone 4-Methylpyrazole
3A Testosterone 6β-OH testosterone Ketoconazole
3A Midazolam 1’-OH midazolam Ketoconazole